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本文报道了一系列抗胆碱能化合物3-甲基-3-氮杂双环[3,3,1]壬-9-酯类α和β异构体的合成。将3-甲基-3-氮杂双环[3,3,1]壬-9-酮还原为相应的醇后,分离成9α和9β两种异构醇,再分别与各种取代羧酸甲酯进行酯交换,而得α和β酯类。对所有产物的立体构型与~1H核磁共振谱的关系进行了讨论。初步药理实验结果表明,除化合物Ⅲ_9,Ⅲ_(10)外,所有化合物均具有较强的中枢抗胆碱能作用,其中6个化合物的抗摈榔碱震颤作用强度接近或超过阿托品,相应的α和β异构体之间作用强度差别较小。
This paper reports the synthesis of a series of α and β isomers of the anticholinergic 3-methyl-3-azabicyclo [3,3,1] nonan-9-ester. After the 3-methyl-3-azabicyclo [3,3,1] nonan-9-one is reduced to the corresponding alcohol, the two isomeric alcohols, 9α and 9β, are separated and reacted with various substituted carboxylic acid methyl Ester transesterification, resulting in α and β esters. The relationship between the stereoconfiguration of all products and ~ 1H NMR was discussed. The results of preliminary pharmacological experiments showed that all the compounds except for compounds Ⅲ_9 and Ⅲ_ (10) had strong central anticholinergic activity. The anti-teichinine tremor intensities of the six compounds were close to or exceeded that of atropine, and the corresponding α There is little difference in the intensity of action between β and β isomers.